Identification

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Name
Memantine
Accession Number
DB01043  (APRD00221)
Type
Small Molecule
Groups
Approved, Investigational
Description

Initially approved by the FDA in 2013, memantine is an N-methyl-D-aspartate (NMDA) receptor antagonist used in the management of Alzheimer's Disease (AD). It is different from many other Alzheimer's Disease medications, as it works by a different mechanism than the cholinesterase enzyme inhibitors normally employed in the management of Alzheimer's disease [2]. Memantine blocks the effects of glutamate, a neurotransmitter in the brain that leads to neuronal excitability and excessive stimulation in Alzheimer's Disease [7].

In 2010, it was estimated that 36 million people worldwide live with Alzheimer's Disease. In 2013, this number increased to 44 million. Almost doubling every 20 years, the prevalence of Alzheimer's Disease is predicted to reach 66 million by 2030 and to 115 million by 2050 [9]. In December 2013, the G8 dementia summit concluded that dementia should be considered a global priority with the objective of developing a cure or a disease-modifying therapy by the year 2025 [8, 9].

Structure
Thumb
Synonyms
  • 1-Amino-3,5-dimethyladamantane
  • 1,3-Dimethyl-5-adamantanamine
  • 3,5-Dimethyl-1-adamantanamine
  • 3,5-Dimethyl-1-aminoadamantane
  • 3,5-Dimethyltricyclo(3.3.1.1(3,7))decan-1-amine
  • Memantina
  • Memantine
  • Memantinum
External IDs
D-145 / DRG-0267
Product Ingredients
IngredientUNIICASInChI Key
Memantine hydrochlorideJY0WD0UA6041100-52-1LDDHMLJTFXJGPI-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act MemantineTablet5 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
Act MemantineTablet10 mgOralActavis Pharma Company2010-02-18Not applicableCanada
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
AxuraTablet, film coated10 mgOralMerz Pharmaceuticals2002-05-17Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-memantineTablet10 mgOralApotex Corporation2011-06-17Not applicableCanada
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
MarixinoTablet, film coated10 mgOralKrka, D.D.2013-04-29Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Memantine and Donepezil Hydrochlorides Extended-releaseMemantine hydrochloride (14 mg/1) + Donepezil hydrochloride (10 mg/1)Capsule, extended releaseOralAmneal Pharmaceuticals LLC2017-02-01Not applicableUs
Memantine and Donepezil Hydrochlorides Extended-releaseMemantine hydrochloride (28 mg/1) + Donepezil hydrochloride (10 mg/1)Capsule, extended releaseOralAmneal Pharmaceuticals LLC2017-02-01Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitOralActavis Pharma, Inc.2015-04-01Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitOralActavis Pharma, Inc.2015-04-01Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitWockhardt2015-09-04Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitWockhardt2015-09-04Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitVivimed Labs Limited2015-09-04Not applicableUs
Memantine HydrochlorideMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitVivimed Labs Limited2015-09-04Not applicableUs
NamendaMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitOralAllergan, Inc.2003-10-16Not applicableUs
NamendaMemantine hydrochloride (5 mg/1) + Memantine hydrochloride (10 mg/1)KitOralAllergan, Inc.2003-10-16Not applicableUs
International/Other Brands
Abixa / Akatinol / Memox
Categories
UNII
W8O17SJF3T
CAS number
19982-08-2
Weight
Average: 179.3018
Monoisotopic: 179.167399677
Chemical Formula
C12H21N
InChI Key
BUGYDGFZZOZRHP-UHFFFAOYSA-N
InChI
InChI=1S/C12H21N/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10/h9H,3-8,13H2,1-2H3
IUPAC Name
3,5-dimethyladamantan-1-amine
SMILES
CC12CC3CC(C)(C1)CC(N)(C3)C2

Pharmacology

Indication

Memantine is used to manage moderate to severe Alzheimer's dementia [Label].

A more recent systemic review and meta-analysis [6] indicates that memantine is beneficial as a first line drug for the treatment of Alzheimer's dementia. Cholinesterase inhibitors may be added to memantine for further beneficial effects on behavioral symptoms and other symptoms of dementia [6].

Associated Conditions
Pharmacodynamics

General effects

This drug inhibits calcium influx into cells that is normally caused by chronic NMDA receptor activation by glutamate [3]. This leads to the improvement of Alzheimer's dementia symptoms, demonstrated by increased cognition and other beneficial central nervous system effects [3].

Effects on neuroplasticity

Like other NMDA receptor antagonists, memantine at high doses can reduce neuronal synaptic plasticity that is involved in learning and memory processes. At lower concentrations, which are normally used in the clinical setting, memantine can enhance neuronal synaptic plasticity in the brain, improve memory, and act as a neuroprotectant against the destruction of neurons caused by excitatory neurotransmitters [2].

Effect on various receptors

Memantine has demonstrated minimal activity for GABA, benzodiazepine, dopamine, adrenergic, histamine, and glycine receptors, as well as voltage-dependent Ca2+, Na+ or K+ channels. This drug has shown antagonist activity at the 5HT3 receptors. Laboratory studies suggest that memantine does not affect the reversible inhibition of the acetylcholinesterase normally caused by donepezil, galantamine, or tacrine [Label].

Mechanism of action

Continuous activation of the N-methyl-D-aspartate (NMDA) receptors in the central nervous system caused by glutamate is thought to cause some of the Alzheimer's disease symptoms. This overactivation is thought to contribute to neurotoxicity due to the excitatory properties of glutamate [7]. The pharmacological effect of memantine likely occurs via the drug's behavior as an uncompetitive (open-channel) NMDA receptor antagonist, preventing glutamate action on this receptor. Memantine has a preference for the NMDA receptor-operated cation channels. Despite these antagonist effects, memantine has not been proven to prevent or retard the neurodegeneration seen in patients diagnosed with Alzheimer’s disease [Label].

TargetActionsOrganism
U5-hydroxytryptamine receptor 3A
antagonist
Humans
UAlpha-7 nicotinic cholinergic receptor subunit
antagonist
Humans
UD(2) dopamine receptor
antagonist
agonist
Humans
UGlutamate receptor ionotropic, NMDA 1
binder
Humans
AGlutamate (NMDA) receptor
antagonist
Humans
UGABA-A receptor (anion channel)
binder
Humans
UGlycine receptors
inhibitor
Absorption

After an oral dose, memantine is well absorbed. Its peak drug concentrations are attained in about 3-7 hours. Memantine shows linear pharmacokinetics when given at normal therapeutic doses. This drug can be taken without regard to food, as there is no effect of food on memantine absorption [Label].

Volume of distribution

The mean volume of distribution of memantine is 9-11 L/kg [Label].

Protein binding

The protein binding for memantine is about 45% [Label].

Metabolism

This drug is partially metabolized in the liver. The hepatic CYP450 enzyme system does not majorly contribute to the metabolism of this drug [Label].

Route of elimination

This drug is mainly excreted in the urine. Approximately 48% of administered memantine is excreted unchanged in urine [Label].

The remainder of the drug is metabolized to three main metabolites. These metabolites are the N-glucuronide conjugate, 6-hydroxy memantine, and 1-nitroso-deaminated memantine, which show minimal NMDA receptor antagonist activity [Label].

Half life

Within the range of 60-100 hours [Label].

The terminal elimination half-life was significantly increased in patients with moderate to severe renal impairment, in comparison with patients with normal renal function [Label]. Exercise caution when this drug is administered to patients with renal dysfunction.

Clearance

This drug is cleared by active tubular secretion in the kidneys. Tubular reabsorption of this drug is pH dependent [Label].

Toxicity

LD50

Oral LD50, mouse 437-498 mg/kg [10] Oral LD50, rat 328-370 mg/kg [10]

Carcinogenesis, Mutagenesis, Impairment of Fertility

No evidence of carcinogenicity was seen in mouse and rat models administered memantine at doses equivalent to supratherapeutic human doses [Label]. Additionally, no genotoxic potential was noted when a battery of assays was performed. No effects on fertility or reproductive performance were noted in rats given to 18 mg/kg/day (equivalent to 9 times the maximum recommended human dose) orally from 14 days preceding mating through gestation and lactation in females, or for 60 preceding mating activity in males animals [Label].

Use in pregnancy

This drug is considered a pregnancy category B drug, meaning no sufficiently controlled and adequate studies of memantine in pregnant women have been performed. This drug should be taken during pregnancy only if the potential benefit justifies the possible fetal risk [Label].

Use in nursing

It is unknown whether memantine is excreted in human milk. Due to that fact that many drugs are found excreted in human milk, caution should be observed when this drug is taken by a nursing mother [Label].

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Memantine.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Memantine.
AbacavirMemantine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarboseAcarbose may decrease the excretion rate of Memantine which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Memantine which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Memantine which could result in a higher serum level.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Memantine.
AcetaminophenAcetaminophen may decrease the excretion rate of Memantine which could result in a higher serum level.
AcetazolamideThe excretion of Memantine can be decreased when combined with Acetazolamide.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Memantine which could result in a higher serum level.
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference
US3391142
General References
  1. Cacabelos R, Takeda M, Winblad B: The glutamatergic system and neurodegeneration in dementia: preventive strategies in Alzheimer's disease. Int J Geriatr Psychiatry. 1999 Jan;14(1):3-47. [PubMed:10029935]
  2. Rogawski MA, Wenk GL: The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease. CNS Drug Rev. 2003 Fall;9(3):275-308. [PubMed:14530799]
  3. Robinson DM, Keating GM: Memantine: a review of its use in Alzheimer's disease. Drugs. 2006;66(11):1515-34. [PubMed:16906789]
  4. Rogawski MA: Low affinity channel blocking (uncompetitive) NMDA receptor antagonists as therapeutic agents--toward an understanding of their favorable tolerability. Amino Acids. 2000;19(1):133-49. [PubMed:11026482]
  5. Rammes G, Rupprecht R, Ferrari U, Zieglgansberger W, Parsons CG: The N-methyl-D-aspartate receptor channel blockers memantine, MRZ 2/579 and other amino-alkyl-cyclohexanes antagonise 5-HT(3) receptor currents in cultured HEK-293 and N1E-115 cell systems in a non-competitive manner. Neurosci Lett. 2001 Jun 22;306(1-2):81-4. [PubMed:11403963]
  6. Kishi T, Matsunaga S, Oya K, Nomura I, Ikuta T, Iwata N: Memantine for Alzheimer's Disease: An Updated Systematic Review and Meta-analysis. J Alzheimers Dis. 2017;60(2):401-425. doi: 10.3233/JAD-170424. [PubMed:28922160]
  7. Brianne Kuns; Dona Varghese (2019). StatPearls: Memantine. StatPearls Publishing.
  8. 135 million people will live with dementia worldwide by 2050 [Link]
  9. Alzheimer's disease international: Global Impact of Dementia 2013 [File]
  10. Memantine Product [File]
External Links
Human Metabolome Database
HMDB0015177
KEGG Drug
D08174
KEGG Compound
C13736
PubChem Compound
4054
PubChem Substance
46506702
ChemSpider
3914
BindingDB
50062599
ChEBI
64312
ChEMBL
CHEMBL807
Therapeutic Targets Database
DAP000493
PharmGKB
PA10364
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Memantine
ATC Codes
N06DA52 — Donepezil and memantineN06DX01 — MemantineN06DA53 — Donepezil, memantine and ginkgo folium
AHFS Codes
  • 28:92.00 — Miscellaneous Central Nervous System Agents
FDA label
Download (604 KB)
MSDS
Download (65.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingOtherAutism Spectrum Conditions/Disorders1
0RecruitingTreatmentStroke, Ischemic / Upper Extremity Weakness1
1Active Not RecruitingTreatmentBrain Cancer1
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailableHealthy Volunteers / Obese, Otherwise Healthy Volunteers1
1CompletedBasic ScienceBioequivalence, AUC, Cmax, Pharmacokinetics1
1CompletedBasic ScienceMajor Depressive Disorder (MDD)1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentTobacco Use Disorders2
1Not Yet RecruitingTreatmentAlzheimer's Disease (AD)1
1RecruitingTreatmentAlzheimer's Disease (AD) / Battery1
1WithdrawnTreatmentAlzheimer's Disease (AD)1
1, 2Active Not RecruitingTreatmentChronic Orthostatic Intolerance / Tachycardia1
1, 2RecruitingHealth Services ResearchSchizophrenic Disorders1
1, 2RecruitingTreatmentStimulants Use Disorder1
2CompletedOtherAlcohol Drinking2
2CompletedSupportive CareCancer, Breast / Colorectal Cancers / Lung Cancers / Prostate Cancer / Tobacco Use Disorders1
2CompletedTreatmentAIDS-Related Dementia Complex / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentAlcohol Abuse / Alcohol Dependence (Primary Condition)1
2CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS)2
2CompletedTreatmentAsperger's / Asperger's Disorder / Autism Spectrum Conditions/Disorders / Autism, Early Infantile / Autistic Disorder / Pediatric Autism / Pervasive Child Development Disorder / Pervasive Developmental Disorder Not Otherwise Specified (PDD-NOS)1
2CompletedTreatmentAsperger's / Asperger's Disorder / Autism Spectrum Conditions/Disorders / Autism, Early Infantile / Autistic Disorder / Pediatric Autism / Pervasive Developmental Disorder Not Otherwise Specified (PDD-NOS)1
2CompletedTreatmentAutism Spectrum Conditions/Disorders1
2CompletedTreatmentAutism, Early Infantile1
2CompletedTreatmentAutism, Early Infantile / Pediatric Autism1
2CompletedTreatmentBipolar Disorder (BD)1
2CompletedTreatmentCocaine-Related Disorders1
2CompletedTreatmentCompulsive Buying1
2CompletedTreatmentDementia Associated With Parkinson's Disease / Diffuse Lewy Body Disease1
2CompletedTreatmentDementias1
2CompletedTreatmentHealthy Volunteers1
2CompletedTreatmentHuntington's Disease (HD)1
2CompletedTreatmentKleptomania1
2CompletedTreatmentMemory Disorders / Memory, Concentration or Attention Problems / Retention Disorders, Cognitive / Subjective Cognitive Impairment1
2CompletedTreatmentObsessive Compulsive Disorder (OCD)1
2CompletedTreatmentOpioid Dependence1
2CompletedTreatmentPain, Neuropathic1
2CompletedTreatmentPathological Gambling1
2CompletedTreatmentPendular Nystagmus Patients With Multiple Sclerosis1
2CompletedTreatmentSchizophrenic Disorders1
2Not Yet RecruitingTreatmentPain, Neuropathic1
2Not Yet RecruitingTreatmentSickle Cell Disorders1
2RecruitingSupportive CareEpendymomas / Germ Cell Tumors / Glioma of Brain / Postsurgical craniopharyngioma1
2RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS) / Frontal Temporal Dementia (FTD)1
2RecruitingTreatmentBipolar Disorder (BD)1
2RecruitingTreatmentDisability, Intellectual / Down Syndrome (DS)1
2RecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
2TerminatedTreatmentAsperger's / Asperger's Disorder / Autism Spectrum Conditions/Disorders / Autism, Early Infantile / Autistic Disorder / Pediatric Autism / Pervasive Developmental Disorder Not Otherwise Specified (PDD-NOS)1
2TerminatedTreatmentDisseminated Sclerosis1
2TerminatedTreatmentGlioblastomas1
2TerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2, 3CompletedTreatmentAlzheimer's Disease (AD) / Major Depressive Disorder (MDD) / Mild Cognitive Impairment (MCI)1
2, 3CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS)1
2, 3CompletedTreatmentBipolar Disorder (BD)1
2, 3CompletedTreatmentHeroin Dependence / Opioid Dependence1
2, 3CompletedTreatmentOpioid Dependence1
2, 3RecruitingTreatmentCognitive Impairments1
2, 3Unknown StatusTreatmentCognition Disorders / Disseminated Sclerosis1
3Active Not RecruitingSupportive CareCognitive Impairments / Metastatic Malignant Neoplasm in the Brain / Solid Neoplasms1
3Active Not RecruitingSupportive CareCognitive/Functional Effects / Metastatic Cancers / Neurologic toxicity / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedNot AvailableAlzheimer's Disease (AD)1
3CompletedTreatmentAlzheimer's Disease (AD)4
3CompletedTreatmentAnxiety Disorders / Obsessive Compulsive Disorder (OCD)1
3CompletedTreatmentAutism Spectrum Conditions/Disorders1
3CompletedTreatmentDementia of the Alzheimer's Type1
3CompletedTreatmentDepression1
3CompletedTreatmentDisseminated Sclerosis1
3CompletedTreatmentFrontotemporal Dementia1
3CompletedTreatmentGeneral Anxiety Disorder, Social Anxiety Disorder1
3CompletedTreatmentHeadache, Tension-Type1
3CompletedTreatmentOpen-angle Glaucoma (OAG)2
3CompletedTreatmentSubstance Abuse1
3Enrolling by InvitationTreatmentAOD Effects and Consequences1
3Enrolling by InvitationTreatmentBipolar Disorder II1
3Not Yet RecruitingTreatmentAutism Spectrum Conditions/Disorders / Autism, Early Infantile / Nonverbal Learning Disability1
3Not Yet RecruitingTreatmentExcitotoxicity / Memantine / Stroke, Ischemic1
3Not Yet RecruitingTreatmentParkinson's Disease (PD)1
3RecruitingTreatmentMetastatic Brain Tumors1
3RecruitingTreatmentSchizophrenic Disorders1
3TerminatedPreventionSchizophrenic Disorders1
3TerminatedTreatmentAlzheimer's Disease (AD)2
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentChronic Schizophrenia1
3Unknown StatusTreatmentFibromyalgia1
4CompletedNot AvailableAlzheimer's Disease (AD)1
4CompletedBasic ScienceAlzheimer's Disease (AD)1
4CompletedTreatmentAlcohol Dependence / Depression1
4CompletedTreatmentAlzheimer Dementia (AD)1
4CompletedTreatmentAlzheimer's Disease (AD)11
4CompletedTreatmentAphasia / Strokes1
4CompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD)1
4CompletedTreatmentAutism Spectrum Conditions/Disorders1
4CompletedTreatmentBinge Eating Disorder (BED)1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentCRP1
4CompletedTreatmentDementia, Alzheimer Type1
4CompletedTreatmentDementias1
4CompletedTreatmentDepression1
4CompletedTreatmentDepression, Bipolar1
4CompletedTreatmentDepression / MCI1
4CompletedTreatmentDepressive Disorders1
4CompletedTreatmentDiffuse Lewy Body Disease / Parkinson's Disease Dementia (PDD)1
4CompletedTreatmentDisseminated Sclerosis1
4CompletedTreatmentDown Syndrome (DS)1
4CompletedTreatmentFrontal Lobe Dementia / Frontotemporal Lobe Dementia / Semantic Dementia1
4CompletedTreatmentFrontotemporal Lobar Degeneration1
4CompletedTreatmentGait Disorders, Neurologic / Parkinson's Disease (PD)1
4CompletedTreatmentOculopalatal Tremor / Pendular Nystagmus1
4CompletedTreatmentOrganic Memory Impairment1
4CompletedTreatmentParkinson's Disease (PD)1
4CompletedTreatmentPhysiological Effects of Drugs1
4CompletedTreatmentPost Traumatic Stress Disorder (PTSD)1
4CompletedTreatmentSchizophrenic Disorders1
4CompletedTreatmentTremor, Essential1
4RecruitingSupportive CareHealthy Volunteers / Schizo Affective Disorder / Schizoaffective Disorders / Schizophrenic Disorders1
4RecruitingTreatmentAlzheimer's Disease (AD)1
4RecruitingTreatmentEpileptic Encephalopathy, Childhood-Onset1
4TerminatedPreventionDelirium / Post-Operative States1
4TerminatedTreatmentAlzheimer's Disease (AD)1
4TerminatedTreatmentMemory Disturbances / Mood1
4TerminatedTreatmentPain NOS1
4TerminatedTreatmentTraumatic Brain Injury (TBI)1
4Unknown StatusTreatmentAlzheimer's Disease (AD) / Dementias1
4Unknown StatusTreatmentAphasia / Strokes1
4Unknown StatusTreatmentDementias1
4Unknown StatusTreatmentHuntington's Disease (HD)1
4Unknown StatusTreatmentModerate to Severe Alzheimer's Disease1
4Unknown StatusTreatmentPost-Operative Pain1
Not AvailableCompletedBasic ScienceHealthy Individuals1
Not AvailableCompletedTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Executive Function Deficits (EFD)1
Not AvailableCompletedTreatmentBipolar Disorder (BD)1
Not AvailableCompletedTreatmentBody Dysmorphic Disorders / Bulimia Nervosa (BN)1
Not AvailableCompletedTreatmentCognitive Impairments / Dementias / Parkinson's Disease (PD)1
Not AvailableCompletedTreatmentDementias1
Not AvailableCompletedTreatmentEpilepsies1
Not AvailableCompletedTreatmentNystagmus / Nystagmus, Pathological1
Not AvailableCompletedTreatmentObsessive Compulsive Disorder (OCD)1
Not AvailableCompletedTreatmentParkinson's Disease (PD)1
Not AvailableCompletedTreatmentSystemic Lupus Erythematosus (SLE)1
Not AvailableCompletedTreatmentTraumatic Brain Injury (TBI)1
Not AvailableRecruitingNot AvailableSchizophrenic Disorders1
Not AvailableUnknown StatusBasic ScienceSpinal Cord Injury, Chronic1
Not AvailableUnknown StatusPreventionMajor Depressive Disorder (MDD)1
Not AvailableUnknown StatusTreatmentAlzheimer's Disease (AD)1
Not AvailableUnknown StatusTreatmentAsperger's Disorder / Autism, Early Infantile / Pervasive Developmental Disorder NOS1
Not AvailableUnknown StatusTreatmentDementias / Down Syndrome (DS) / Learning Disabilities1
Not AvailableUnknown StatusTreatmentFragile X Premutation Carriers / Fragile X-Associated Tremor/Ataxia Syndrome1
Not AvailableWithdrawnSupportive CareEpilepsies1
Not AvailableWithdrawnTreatmentAttention Deficit Disorder With Hyperactivity (ADHD) / Executive Function Deficits (EFD's)1
Not AvailableWithdrawnTreatmentMajor Depressive Disorder (MDD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bryant Ranch Prepack
  • Cardinal Health
  • Coupler Enterprises Inc.
  • Forest Laboratories Inc.
  • Forest Pharmaceuticals
  • Lake Erie Medical and Surgical Supply
  • Lundbeck Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Stat Rx Usa
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletOral5 mg
TabletOral10 mg
Tablet, film coatedOral10 mg
Tablet, film coatedOral20 mg
Capsule, extended releaseOral
Capsule, extended releaseOral21 mg/1
Kit
LiquidOral2 mg/1mL
SolutionOral2 mg/1mL
Tablet, coatedOral10 mg/1
Tablet, coatedOral5 mg/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
KitOral
TabletOral10 mg/1
TabletOral5 mg/1
Capsule, extended releaseOral14 mg/1
Capsule, extended releaseOral28 mg/1
Capsule, extended releaseOral7 mg/1
CapsuleOral
TabletOral5.0 mg
Prices
Unit descriptionCostUnit
Namenda 10 mg tablet3.38USD tablet
Namenda 5 mg tablet3.32USD tablet
Namenda 5-10 mg titration pk3.32USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2426492No2006-10-032023-05-08Canada
US8173708Yes2012-05-082026-05-22Us
US8283379Yes2012-10-092026-05-22Us
US8362085Yes2013-01-292026-05-22Us
US8039009Yes2011-10-182029-09-24Us
US8329752Yes2012-12-112026-05-22Us
US8598233Yes2013-12-032026-05-22Us
US8168209Yes2012-05-012026-05-22Us
US8338486No2012-12-252025-11-22Us
US8058291No2011-11-152029-12-05Us
US8580858No2013-11-122025-11-22Us
US8338485No2012-12-252025-11-22Us
US8293794No2012-10-232025-11-22Us
US5061703Yes1991-10-292015-10-11Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)153https://www.lookchem.com/Memantine/
boiling point (°C)239.8https://www.lookchem.com/Memantine/
water solubilitysoluble in waterhttps://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021627lbl.pdf
logP3.28https://www.lundbeck.com/upload/ca/en/files/pdf/pm/Ebixa.pdf
pKa10.27https://www.lundbeck.com/upload/ca/en/files/pdf/pm/Ebixa.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0455 mg/mLALOGPS
logP3.31ALOGPS
logP2.07ChemAxon
logS-3.6ALOGPS
pKa (Strongest Basic)10.7ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area26.02 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity54.49 m3·mol-1ChemAxon
Polarizability21.82 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9939
Blood Brain Barrier+0.9823
Caco-2 permeable+0.6082
P-glycoprotein substrateNon-substrate0.6403
P-glycoprotein inhibitor INon-inhibitor0.82
P-glycoprotein inhibitor IINon-inhibitor0.7555
Renal organic cation transporterNon-inhibitor0.7774
CYP450 2C9 substrateNon-substrate0.8213
CYP450 2D6 substrateNon-substrate0.6153
CYP450 3A4 substrateNon-substrate0.5319
CYP450 1A2 substrateNon-inhibitor0.9327
CYP450 2C9 inhibitorNon-inhibitor0.9281
CYP450 2D6 inhibitorNon-inhibitor0.872
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6795
Ames testNon AMES toxic0.6945
CarcinogenicityNon-carcinogens0.7426
BiodegradationNot ready biodegradable0.9633
Rat acute toxicity2.3455 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9839
hERG inhibition (predictor II)Non-inhibitor0.6818
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03e9-0900000000-65172d14e0f6b9102d73
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0900000000-ce475f103d528ff4d342
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0900000000-1c9199c5cf1c902223ae
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-08fr-0900000000-1bac817f714e7eec7488
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-2900000000-eb58e236084a93a3d37b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-4900000000-5a87d54400c3e9720ad0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052f-9500000000-95eb2b63a2392449ec4a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-9100000000-608b372857aacd60eb61
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00kf-9000000000-f283a81168372575c2aa
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0900000000-bbf1127413d0f995a000

Taxonomy

Description
This compound belongs to the class of organic compounds known as monoalkylamines. These are organic compounds containing an primary aliphatic amine group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Monoalkylamines
Alternative Parents
Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Organopnictogen compound / Hydrocarbon derivative / Primary aliphatic amine / Aliphatic homopolycyclic compound
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
adamantanes, primary aliphatic amine (CHEBI:64312)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated potassium channel activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
Molecular Weight
55279.835 Da
References
  1. Rammes G, Rupprecht R, Ferrari U, Zieglgansberger W, Parsons CG: The N-methyl-D-aspartate receptor channel blockers memantine, MRZ 2/579 and other amino-alkyl-cyclohexanes antagonise 5-HT(3) receptor currents in cultured HEK-293 and N1E-115 cell systems in a non-competitive manner. Neurosci Lett. 2001 Jun 22;306(1-2):81-4. [PubMed:11403963]
  2. Nisijima K, Shioda K, Yoshino T, Takano K, Kato S: Memantine, an NMDA antagonist, prevents the development of hyperthermia in an animal model for serotonin syndrome. Pharmacopsychiatry. 2004 Mar;37(2):57-62. doi: 10.1055/s-2004-815526. [PubMed:15048612]
  3. Memantine FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Not Available
Specific Function
Not Available
Gene Name
CHRNA7
Uniprot ID
Q693P7
Uniprot Name
Alpha-7 nicotinic cholinergic receptor subunit
Molecular Weight
2987.635 Da
References
  1. Aracava Y, Pereira EF, Maelicke A, Albuquerque EX: Memantine blocks alpha7* nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons. J Pharmacol Exp Ther. 2005 Mar;312(3):1195-205. Epub 2004 Nov 2. [PubMed:15522999]
  2. Maskell PD, Speder P, Newberry NR, Bermudez I: Inhibition of human alpha 7 nicotinic acetylcholine receptors by open channel blockers of N-methyl-D-aspartate receptors. Br J Pharmacol. 2003 Dec;140(7):1313-9. doi: 10.1038/sj.bjp.0705559. [PubMed:14645141]
  3. Pohanka M: Alpha7 nicotinic acetylcholine receptor is a target in pharmacology and toxicology. Int J Mol Sci. 2012;13(2):2219-38. doi: 10.3390/ijms13022219. Epub 2012 Feb 17. [PubMed:22408449]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Seeman P, Caruso C, Lasaga M: Memantine agonist action at dopamine D2High receptors. Synapse. 2008 Feb;62(2):149-53. [PubMed:18000814]
  2. Serra G, Demontis F, Serra F, De Chiara L, Spoto A, Girardi P, Vidotto G, Serra G: Memantine: New prospective in bipolar disorder treatment. World J Psychiatry. 2014 Dec 22;4(4):80-90. doi: 10.5498/wjp.v4.i4.80. [PubMed:25540723]
  3. Nakaya K, Nakagawasai O, Arai Y, Onogi H, Sato A, Niijima F, Tan-No K, Tadano T: Pharmacological characterizations of memantine-induced disruption of prepulse inhibition of the acoustic startle response in mice: involvement of dopamine D2 and 5-HT2A receptors. Behav Brain Res. 2011 Mar 17;218(1):165-73. doi: 10.1016/j.bbr.2010.11.053. Epub 2010 Dec 3. [PubMed:21130810]
  4. Mancini M, Ghiglieri V, Bagetta V, Pendolino V, Vannelli A, Cacace F, Mineo D, Calabresi P, Picconi B: Memantine alters striatal plasticity inducing a shift of synaptic responses toward long-term depression. Neuropharmacology. 2016 Feb;101:341-50. doi: 10.1016/j.neuropharm.2015.10.015. Epub 2015 Dec 3. [PubMed:26471421]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
Curator comments
This is a potential target. There are limited data regarding this target in the literature.
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...
Gene Name
GRIN1
Uniprot ID
Q05586
Uniprot Name
Glutamate receptor ionotropic, NMDA 1
Molecular Weight
105371.945 Da
References
  1. Kotermanski SE, Wood JT, Johnson JW: Memantine binding to a superficial site on NMDA receptors contributes to partial trapping. J Physiol. 2009 Oct 1;587(Pt 19):4589-604. doi: 10.1113/jphysiol.2009.176297. Epub 2009 Aug 17. [PubMed:19687120]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Voltage-gated cation channel activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...

Components:
References
  1. Robinson DM, Keating GM: Memantine: a review of its use in Alzheimer's disease. Drugs. 2006;66(11):1515-34. [PubMed:16906789]
  2. Cacabelos R, Takeda M, Winblad B: The glutamatergic system and neurodegeneration in dementia: preventive strategies in Alzheimer's disease. Int J Geriatr Psychiatry. 1999 Jan;14(1):3-47. [PubMed:10029935]
  3. Rogawski MA, Wenk GL: The neuropharmacological basis for the use of memantine in the treatment of Alzheimer's disease. CNS Drug Rev. 2003 Fall;9(3):275-308. [PubMed:14530799]
  4. Memantine FDA label [File]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
Curator comments
The binding of memantine to this target is believed to be low to negligible.
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
References
  1. Molinaro G, Battaglia G, Riozzi B, Di Menna L, Rampello L, Bruno V, Nicoletti F: Memantine treatment reduces the expression of the K(+)/Cl(-) cotransporter KCC2 in the hippocampus and cerebral cortex, and attenuates behavioural responses mediated by GABA(A) receptor activation in mice. Brain Res. 2009 Apr 10;1265:75-9. doi: 10.1016/j.brainres.2009.02.016. Epub 2009 Feb 21. [PubMed:19236854]
  2. Memantine FDA label [File]
7. Glycine receptors
Kind
Protein group
Organism
Not Available
Pharmacological action
Unknown
Actions
Inhibitor
References
  1. Xia P, Chen HS, Zhang D, Lipton SA: Memantine preferentially blocks extrasynaptic over synaptic NMDA receptor currents in hippocampal autapses. J Neurosci. 2010 Aug 18;30(33):11246-50. doi: 10.1523/JNEUROSCI.2488-10.2010. [PubMed:20720132]
  2. Limapichat W, Yu WY, Branigan E, Lester HA, Dougherty DA: Key binding interactions for memantine in the NMDA receptor. ACS Chem Neurosci. 2013 Feb 20;4(2):255-60. doi: 10.1021/cn300180a. Epub 2012 Dec 7. [PubMed:23421676]
  3. Memantine FDA label [File]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Data are limited to the results of an in vitro study. Current information in the literature is limited.
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Micuda S, Mundlova L, Anzenbacherova E, Anzenbacher P, Chladek J, Fuksa L, Martinkova J: Inhibitory effects of memantine on human cytochrome P450 activities: prediction of in vivo drug interactions. Eur J Clin Pharmacol. 2004 Oct;60(8):583-9. doi: 10.1007/s00228-004-0825-1. Epub 2004 Sep 16. [PubMed:15378224]
  2. Korhonen LE, Turpeinen M, Rahnasto M, Wittekindt C, Poso A, Pelkonen O, Raunio H, Juvonen RO: New potent and selective cytochrome P450 2B6 (CYP2B6) inhibitors based on three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis. Br J Pharmacol. 2007 Apr;150(7):932-42. doi: 10.1038/sj.bjp.0707173. Epub 2007 Feb 26. [PubMed:17325652]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Data are based on the results of an in vitro study. Current information in the literature regarding this enzyme action is limited.
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Micuda S, Mundlova L, Anzenbacherova E, Anzenbacher P, Chladek J, Fuksa L, Martinkova J: Inhibitory effects of memantine on human cytochrome P450 activities: prediction of in vivo drug interactions. Eur J Clin Pharmacol. 2004 Oct;60(8):583-9. doi: 10.1007/s00228-004-0825-1. Epub 2004 Sep 16. [PubMed:15378224]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
There is limited current data available on this enzyme inhibition, with the exception of one in vitro study.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Micuda S, Mundlova L, Anzenbacherova E, Anzenbacher P, Chladek J, Fuksa L, Martinkova J: Inhibitory effects of memantine on human cytochrome P450 activities: prediction of in vivo drug interactions. Eur J Clin Pharmacol. 2004 Oct;60(8):583-9. doi: 10.1007/s00228-004-0825-1. Epub 2004 Sep 16. [PubMed:15378224]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
This transporter is a potential transporter and has not been confirmed.
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Busch AE, Karbach U, Miska D, Gorboulev V, Akhoundova A, Volk C, Arndt P, Ulzheimer JC, Sonders MS, Baumann C, Waldegger S, Lang F, Koepsell H: Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine. Mol Pharmacol. 1998 Aug;54(2):342-52. [PubMed:9687576]
  2. Muller F, Weitz D, Derdau V, Sandvoss M, Mertsch K, Konig J, Fromm MF: Contribution of MATE1 to Renal Secretion of the NMDA Receptor Antagonist Memantine. Mol Pharm. 2017 Sep 5;14(9):2991-2998. doi: 10.1021/acs.molpharmaceut.7b00179. Epub 2017 Aug 2. [PubMed:28708400]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
This is a potential transporter and has not been confirmed.
General Function
Solute:proton antiporter activity
Specific Function
Involved in pH regulation to eliminate acids generated by active metabolism or to counter adverse environmental conditions. Major proton extruding system driven by the inward sodium ion chemical gr...
Gene Name
SLC9A1
Uniprot ID
P19634
Uniprot Name
Sodium/hydrogen exchanger 1
Molecular Weight
90762.13 Da
References
  1. Mehta DC, Short JL, Nicolazzo JA: Memantine transport across the mouse blood-brain barrier is mediated by a cationic influx H+ antiporter. Mol Pharm. 2013 Dec 2;10(12):4491-8. doi: 10.1021/mp400316e. Epub 2013 Oct 29. [PubMed:24098999]
  2. Mehta DC, Short JL, Nicolazzo JA: Reduced CNS exposure of memantine in a triple transgenic mouse model of Alzheimer's disease assessed using a novel LC-MS technique. J Pharm Biomed Anal. 2013 Nov;85:198-206. doi: 10.1016/j.jpba.2013.07.027. Epub 2013 Jul 30. [PubMed:23954439]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
This is a potential transporter and has not been confirmed.
General Function
Symporter activity
Specific Function
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without...
Gene Name
SLC22A4
Uniprot ID
Q9H015
Uniprot Name
Solute carrier family 22 member 4
Molecular Weight
62154.48 Da
References
  1. Mehta DC, Short JL, Nicolazzo JA: Memantine transport across the mouse blood-brain barrier is mediated by a cationic influx H+ antiporter. Mol Pharm. 2013 Dec 2;10(12):4491-8. doi: 10.1021/mp400316e. Epub 2013 Oct 29. [PubMed:24098999]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
This is a potential transporter and has not been confirmed.
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. Muller F, Weitz D, Derdau V, Sandvoss M, Mertsch K, Konig J, Fromm MF: Contribution of MATE1 to Renal Secretion of the NMDA Receptor Antagonist Memantine. Mol Pharm. 2017 Sep 5;14(9):2991-2998. doi: 10.1021/acs.molpharmaceut.7b00179. Epub 2017 Aug 2. [PubMed:28708400]

Drug created on June 13, 2005 07:24 / Updated on April 22, 2019 17:13